El-Sawy Eslam R, Abdel-Aziz Mohamed S, Kirsch Gilbert
Chemistry of Natural Compounds Department, National Research Centre, Dokki, 12622, Giza, Egypt.
Microbial Chemistry Department, Biotechnology Research Institute, National Research Centre, Dokki, 12622, Giza, Egypt.
Curr Org Synth. 2025;22(3):328-341. doi: 10.2174/0115701794325027240827043203.
Natural products, with their various sources from plants, marine organisms, and microorganisms, are considered a key source and inspiration for medicines and continue to be so. Indole alkaloids are a class of alkaloids and represent a large subunit of natural products. Indole alkaloids of biological importance are numerous and cover a wide range of pharmaceutical applications, including anticancer, antiviral, antimicrobial, anti-inflammatory, and antioxidant. Obtaining natural, biologically active indole compounds involves isolating them from their natural sources or preparing them synthetically. 3-Substituted indoles represent an emerging structural class of marine alkaloids based on their high degree of biological activity. 3-Acetyl indole is an important core used as a starting material for synthesizing many bioactive indole alkaloids. (5-Indole)oxazole alkaloids, β-carboline alkaloids, bis-indole alkaloids, chuangxinmycin, meridianine, and (±) indolemycin are the most important indole alkaloids that are prepared starting from 3-acety indole. The present review provides comprehensive information on the structures and the synthesis of bioactive indole alkaloids utilizing 3-acetyl indole and its derivatives as starting compounds. Additionally, it also spotlights the diverse biological activities of these compounds.
天然产物来源于植物、海洋生物和微生物等多种来源，被认为是药物的关键来源和灵感源泉，并且一直如此。吲哚生物碱是一类生物碱，是天然产物的一个大亚基。具有生物学重要性的吲哚生物碱众多，涵盖广泛的药物应用，包括抗癌、抗病毒、抗菌、抗炎和抗氧化等。获得天然的、具有生物活性的吲哚化合物涉及从其天然来源中分离或通过合成制备。3-取代吲哚基于其高度的生物活性，代表了一类新兴的海洋生物碱结构类型。3-乙酰基吲哚是一种重要的核心物质，用作合成许多生物活性吲哚生物碱的起始原料。（5-吲哚基）恶唑生物碱、β-咔啉生物碱、双吲哚生物碱、创新霉素、子午线碱和（±）吲哚霉素是从3-乙酰基吲哚开始制备的最重要的吲哚生物碱。本综述提供了关于以3-乙酰基吲哚及其衍生物为起始化合物的生物活性吲哚生物碱的结构和合成的全面信息。此外，还突出了这些化合物的多种生物活性。
